部份中文帕博西尼处方资料（仅供参考）
英文名：Palbociclib
商品名：IBRANCE Capsules
中文名：帕博西尼胶囊
生产商：辉瑞公司
产品简介
辉瑞开发的抗癌新药帕博西尼（palbociclib，IBRANCE）联合来曲唑作为内分泌基础的一线疗法，治疗绝经期女性雌激素受体2阴性的晚期乳腺癌患者。每个用于治疗ER+/HER2-绝经后晚期乳腺癌。Palbociclib （帕博西尼）较来曲唑可使乳腺癌无进展生存期延长一倍，是乳腺癌患者的新希望，疗效获得突破。完全可以取代来曲唑的临床用药。
Palbociclib（帕博西尼）是全球首个CDK4/6激酶抑制剂上市，帕博西尼 （palbociclib）是一种实验性、口服、靶向性 CDK4/6 抑制剂，能够选择性抑制细胞周期蛋白依赖性激酶4和6（CDK4/6），恢复细胞周期控制，阻断肿瘤细胞增殖。细胞周期失控是癌症的一个标志性特征，CDK4/6 在许多癌症中均过度活。
イブランスカプセル25mg/イブランスカプセル125mg
药物分类名称
抗肿瘤药（CDK4/6抑制剂）
批准日期：2017年12月
商標名
IBRANCE Capsules
一般名：パルボシクリブ（Palbociclib）
化学名：6-Acetyl-8-cyclopentyl-5-methyl-2-｛［5-（piperazin-1-yl）pyridin-2-yl］amino｝pyrido［2,3-d］pyrimidin-7（8H）-one
分子式：C24H29N7O2
分子量；447.53
構造式
性状
Parvociclib是一种黄色至橙色粉末。难以溶于N，N-二甲基乙酰胺，它极难溶于乙醇（99.5）和甲醇，几乎不溶于水。
分配系数（log D）0.99（pH 7.4,1-辛醇/水）
批准条件
制定药品风险管理计划并适当实施。
药用药理学
1.抗肿瘤作用
Parvociclib抑制源自人乳腺癌的T47D和MCF7细胞系的增殖。此外，在用人乳腺癌衍生的ZR-75-1细胞系皮下移植的严重联合免疫缺陷小鼠中肿瘤生长被抑制。
2.行动机制
Parvociclib是一种低分子量化合物，对细胞周期蛋白依赖性激酶（CDKs）4和6具有抑制活性。认为parvociclib抑制CDK 4/6和细胞周期蛋白D复合物的活性，通过抑制视网膜母细胞瘤（Rb）蛋白的磷酸化来抑制细胞周期进程，并抑制肿瘤生长 已经完成了。
适应症
不能手术或复发的乳腺癌
用法与用量
与内分泌治疗相结合，通常每天一次125mg，作为parvociclib口服给予成人，连续3周，然后停药1周。以此为循环重复给药。另外，根据患者的状况进行减重。
临床结果
1.国际III期III期HR阳性和HER 2阴性试验以及不能手术或复发的绝经后乳腺癌患者，无先天性乳腺癌内分泌治疗史
HR-阳性和HER2阴性，不能手术的或复发的绝经后乳腺癌666箱子没有内分泌治疗史（包括46案件日语）对称地相对于晚期乳腺癌，这种药物+来曲唑组合投与安慰剂+一项随机，双盲，平行的组-组，国际联合III期试验，以检查来曲唑联合给药的有效性。这种药物，为125mg作为起始剂量之一每日连续3周口服给药后休息一周，来曲唑一度每日2.5毫克连续给药。
中位无进展存活为主要终点，在药物+来曲唑24.8个月，在安慰剂+来曲唑14.5个月，风险比0.576（95％置信区间：0.463,0.718;一个层在另一个log-rank检验p <0.000001）观察在药物+来曲唑的统计学显著无进展生存期的延长。
2.国际III期III期HR阳性和HER 2阴性试验，针对对内分泌治疗有抵抗力的不能手术或复发的乳腺癌患者
对于HR阳性和HER2阴性，521名患者（包括35名日本人）无法手术或复发的乳腺癌患者对内分泌治疗有抗性（无论绝经状态如何），均使用该药物加氟维司群治疗 一项随机，双盲，平行的组-组，国际联合III期试验进行，以检查安慰剂+氟维司群联合用药的有效性。对于该药物，口服给药后连续3周每天一次125mg作为起始剂量，连续3周，第一次，2周，4周，此后每4周给予氟维司群500mg。 戈舍瑞林同时给予绝经前和围绝经期患者。
在中期分析时（2014年12月5日停产）确认了无进展生存期（主要终点）的显着延长，满足预定义的取消标准，并且该研究已经停止。该药物+氟维司群组中位无进展生存期为9.2个月，安慰剂组+氟维司群组为3.8个月，风险比为0.422（95％置信区间：0.318,0.560; 在p <0.000001）的情况下，在该药物+氟维司群组中观察到统计学上显着的无进展存活。
包装
胶囊
25毫克：50粒胶囊（10粒×5 PTP）
125毫克：21粒（7粒×3 PTP）
制造和销售（进口）
辉瑞公司
注：以上中文处方资料不够完整，使用者以原处方资料为准。
完整说明资料附件：
http://www.info.pmda.go.jp/go/pack/4291051M1021_1_04/?view=frame&style=SGML&lang=ja
IBRANCE Capsules 125mg（Palbociclib）
Brand name:IBRANCE Capsules 125mg
Active ingredient:Palbociclib
Dosage form:reddish-brown/reddish-brown capsule,
major axis: 21.7 mm, minor axis: 7.6 mm
Print on wrapping:イブランス, 125mg, IBRANCE, Pfizer, PBC 125
Effects of this medicine
This medicine suppresses tumor growth by inhibiting cyclin dependent kinases 4 and 6 (CDK 4/6), and blockingprogression of the cell cycle.
It is usually used to treat unresectable or recurrent breast cancer.
Before using this medicine, be sure to tell your doctor and pharmacist
• If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines.
If you have liver dysfunction.
• If you are pregnant, possibly pregnant or breastfeeding.
• If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinaleffects. Beware of over-the-counter medicines and dietary supplements as well as other prescriptionmedicines.)
Dosing schedule (How to take this medicine)
• Your dosing schedule prescribed by your doctor is (( to be written by a healthcare professional ))
• In combination with endocrine therapy, in general, for adults, take 1 capsule (125 mg of the active ingredient)at a time, once a day after a meal for 3 consecutive weeks and then stop for 1 week. This treatment cycle isrepeated. The dosage may be decreased according to the condition. Strictly follow the instructions.
• If you miss a dose, skip the missed dose and take a dose at the regular time on the next day. You should nevertake two doses at one time.
• If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist.
• Do not stop taking this medicine unless your doctor instructs you to do so.
Precautions while taking this medicine
• Avoid taking any food containing St. John's wort, since it may diminish medicinal effects.
• Avoid taking grapefruit juice with this medicine, since it may intensify the therapeutic effects of this medicine.
• If you or your partner have a possibility of pregnancy, avoid pregnancy while you are taking this medicine andfor a certain period after you discontinue this medicine.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include alopecia, fatigue, stomatitis, nausea, joint pain, anemia,infection, hot flush, diarrhea, asthenia and rash.If any of these symptoms occur, consult with your doctor orpharmacist.
The symptoms described below are rarely seen as initial symptoms of the adversereactions indicated in brackets.If any of these symptoms occur, stop taking this
medicine and see your doctor immediately.
• anemia, fever, bleeding/bruise [myelosuppression]
The above symptoms do not describe all the adverse reactions to this medicine.
Consult with your doctor or pharmacist if you notice any symptoms of concern otherthan those listed above.
Storage conditions and other information
• Keep out of reach of children. Store away from direct sunlight, heat and moisture.
• Discard the remainder. Do not store them. If you dispose of unused medicines, seek advice of your pharmacistor healthcare provider about proper disposal of them.
Internal
Published: 11/2017
The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approvaldetails may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It isimportant to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response,patients should understand their medication and cooperate with the treatment.